CONTROLLED RELEASE DOSAGE FORMS
The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.
1 . A controlled release oral dosage form comprising:
a. an immediate release core, comprising about 1000 mg of metformin hydrochloride; and
b. a controlled release coating surrounding said core,
wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus II (Paddle Apparatus) method at 50 rpm, in 900 mL water and at about 37° C., such that nor more than about 29% of the metformin hydrochloride is released after about 1 hour and not more than about 41% of the metformin hydrochloride is released after about 3 hours.
2 . The controlled release oral dosage form according to claim 1 , wherein said dosage form releases no more than about 52% of the metformin hydrochloride after about 4 hours.
3 . The controlled release oral dosage form according to claim 1 , wherein said dosage form releases no less than about 85% of the metformin hydrochloride after about 12 hours.
4 . A controlled release oral dosage form comprising:
a. an immediate release core, comprising about 1000 mg of metformin hydrochloride; and
b. a controlled release coating surrounding said core,
wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that between about 18% and about 29% of the metformin hydrochloride is released after about 2 hours, between about 34% and about 50% of the metformin hydrochloride is released after about 4 hours, and between about 67% and about 78% of the metformin hydrochloride is released after about 8 hours.
5 . The controlled release oral dosage form according to claim 4 , wherein said dosage form releases more than about 83% of the metformin hydrochloride after about 12 hours.
6 . A controlled release oral dosage form comprising:
a. an immediate release core, comprising about 1000 mg of metformin hydrochloride; and
b. a controlled release coating surrounding said core,
wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that not more than about 30% of the metformin hydrochloride is released after about 2 hours and not more than about 50% of the metformin hydrochloride is released after about 4 hours.
7 . The controlled release oral dosage form according to claim 6 , wherein said dosage form releases no more than about 78% of the metformin hydrochloride after about 8 hours.
8 . The controlled release oral dosage form according to claim 7 , wherein said dosage form releases no more than about 83% of the metformin hydrochloride after about 12 hours.
9 . The controlled release oral dosage form according to claim 1 , wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that between about 18% and about 29% of the metformin hydrochloride is released after about 2 hours.
10 . The controlled release oral dosage form according to claim 9 , wherein between about 34% and about 50% of the metformin hydrochloride is released after about 4 hours.
11 . A controlled release oral dosage form according to claim 10 , wherein between about 67% and about 78% of the metformin hydrochloride is released after about 8 hours.
12 . The controlled release oral dosage form according to claim 3 , wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that between about 18% and about 29% of the metformin hydrochloride is released after about 2 hours.
13 . The controlled release oral dosage form according to claim 12 , wherein between about 34% and about 50% of the metformin hydrochloride is released after about 4 hours.
14 . The controlled release oral dosage form according to claim 13 , wherein between about 67% and about 78% of the metformin hydrochloride is released after about 8 hours.
15 . The controlled release oral dosage form according to claim 5 , wherein said dosage form provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that between about 18% and about 29% of the metformin hydrochloride is released after about 2 hours.
16 . The controlled release oral dosage form according to claim 15 , wherein between about 34% and about 50% of the metformin hydrochloride is released after about 4 hours.
17 . The controlled release oral dosage form according to claim 16 , wherein between about 67% and about 78% of the metformin hydrochloride is released after about 8 hours.